Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, University of Liège, 4000 Liège, Belgium; Medicinal Organic Chemistry Laboratory (MOCL), School of Pharmacy, Faculté des Sciences de la Santé, Université d'Abomey-Calavi, Campus du Champ de Foire, Cotonou, Benin.
Laboratory of Pharmaceutical Technology and Biopharmacy, CIRM, University of Liège, 4000 Liège, Belgium.
Int J Pharm. 2022 Sep 25;625:122111. doi: 10.1016/j.ijpharm.2022.122111. Epub 2022 Aug 13.
Silicones, more specifically those of the polydimethylsiloxane type, have been widely used in the pharmaceutical industry for decades, particularly in topical applications. In the dermatological field, in addition to provide undeniable textural and sensory benefits, they can play important functions in the physicochemical properties, stability and biopharmaceutical behavior of these formulations. However, despite the notable advances that can be attributed to the family of silicones, the reputation of these compounds is quite bad. Indeed, silicones, even if they derive from sand, are synthetic compounds. Moreover, they are not biodegradable. They flow into our wastewater and oceans, accumulating in the fauna and flora. This obviously raises many concerns in the common imagination. Do silicones represent a danger for our environment? Should the human species worry about long term toxic effects? Are the claimed benefits really that important? After exploring the various applications of silicone excipients in topical dermatological formulations with a special focus on recent advances which open breathtaking prospects for dermatological applications, this paper shed light on the specific challenges involved in preparation of silicone-based drug as well as, the in vivo behavior of these polymers, the toxicological and environmental risks associated with their application.
硅酮,特别是聚二甲基硅氧烷类型的硅酮,已在制药行业中广泛使用了几十年,特别是在局部应用中。在皮肤科领域,除了提供不可否认的质地和感官益处外,它们还可以在这些制剂的物理化学性质、稳定性和生物制药行为中发挥重要作用。然而,尽管硅酮家族取得了显著的进展,但这些化合物的声誉却相当不佳。事实上,硅酮即使来源于沙子,也是合成化合物。此外,它们不可生物降解。它们会流入我们的废水和海洋,在动物群和植物群中积累。这在普通想象中显然引起了许多关注。硅酮对我们的环境构成威胁吗?人类物种是否应该担心长期的毒性影响?声称的好处真的那么重要吗?在探讨了硅酮赋形剂在局部皮肤科制剂中的各种应用,特别关注了为皮肤科应用开辟广阔前景的最新进展之后,本文阐明了制备基于硅酮的药物以及这些聚合物在体内的行为所涉及的具体挑战,以及与它们的应用相关的毒理学和环境风险。